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Decrease of serum angiotensin converting enzyme activity after discontinuation of captopril treatment.

T Forslund, I Tikkanen, F Fyhrquist

Acta Pharmacologica Et Toxicologica

|July 1, 1983

Summary

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Captopril treatment reversibly increases rat serum angiotensin-converting enzyme (ACE) biosynthesis. Serum ACE activity returns to baseline levels within 12 days of drug withdrawal, indicating a reversible effect.

Area of Science:

Pharmacology
Biochemistry
Physiology

Background:

Angiotensin-converting enzyme (ACE) plays a crucial role in the renin-angiotensin system.
ACE inhibitors, like captopril, are widely used to treat hypertension and heart failure.
Understanding the reversibility of ACE modulation is important for clinical practice.

Purpose of the Study:

To investigate the reversibility of captopril-induced changes in serum and lung ACE activity and concentration in rats.
To determine the half-life of serum ACE activity after captopril discontinuation.

Main Methods:

Wistar rats were treated with captopril (30 mg/kg/day) for six weeks.
Serum ACE activity was measured at baseline and at 3, 6, and 12 days post-treatment.
Lung ACE concentration in plasma membranes and homogenates was assessed 12 days after captopril withdrawal.

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Main Results:

Serum ACE activity increased approximately three-fold during captopril treatment.
The estimated half-life of serum ACE activity after captopril withdrawal was 72 hours.
No significant differences in lung ACE concentration were observed between treated and control rats 12 days after discontinuation.

Conclusions:

Captopril-induced ACE biosynthesis in rats is reversible upon drug withdrawal.
Serum ACE activity normalizes within approximately 12 days after cessation of captopril treatment.
Lung ACE concentration remains unaffected long-term after captopril discontinuation.